76246-92-9Relevant academic research and scientific papers
Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer
Nagasawa, Johnny,Govek, Steven,Kahraman, Mehmet,Lai, Andiliy,Bonnefous, Celine,Douglas, Karensa,Sensintaffar, John,Lu, Nhin,Lee, Kyoungjin,Aparicio, Anna,Kaufman, Josh,Qian, Jing,Shao, Gang,Prudente, Rene,Joseph, James D.,Darimont, Beatrice,Brigham, Daniel,Maheu, Kate,Heyman, Richard,Rix, Peter J.,Hager, Jeffrey H.,Smith, Nicholas D.
, p. 7917 - 7928 (2018/09/06)
About 75% of breast cancers are estrogen receptor alpha (ER-α) positive, and women typically initially respond well to antihormonal therapies such as tamoxifen and aromatase inhibitors, but resistance often emerges. Fulvestrant is a steroid-based, selective estrogen receptor degrader (SERD) that both antagonizes and degrades ER-α and shows some activity in patients who have progressed on antihormonal agents. However, fulvestrant must be administered by intramuscular injections that limit its efficacy. We describe the optimization of ER-α degradation efficacy of a chromene series of ER modulators resulting in highly potent and efficacious SERDs such as 14n. When examined in a xenograft model of tamoxifen-resistant breast cancer, 14n (ER-α degradation efficacy = 91%) demonstrated robust activity, while, despite superior oral exposure, 15g (ER-α degradation efficacy = 82%) was essentially inactive. This result suggests that optimizing ER-α degradation efficacy in the MCF-7 cell line leads to compounds with robust effects in models of tamoxifen-resistant breast cancer derived from an MCF-7 background.
Polyaniline-supported zinc oxide (ZnO) nanoparticles: An active and stable heterogeneous catalyst for the Friedel-Crafts acylation reaction
Rezaei, Seyed Jamal Tabatabaei,Nabid, Mohammad Reza,Hosseini, Seyedeh Zahra,Abedi, Mahvash
experimental part, p. 1432 - 1444 (2012/04/17)
We report herein the synthesis of zinc oxide (ZnO) nanoparticles incorporating a polyaniline (PANI) matrix in aqueous medium and its catalytic performance toward Friedel-Crafts acylation reactions. The acylation reactions demonstrate that polyaniline/ nano-ZnO composites are very active catalysts and are able to activate the reactant at ambient temperature. The obtained nanocatalyst was characterized by Fourier transform-infrared, scanning electron microscopy, transmission electron microscopy, Brunauer-Emmett-Teller, X-ray diffraction, and particle-size analysis techniques. The catalyst was reusable for five cycles without appreciable loss in activity. Copyright Taylor & Francis Group, LLC.
Palladium-catalyzed carbonylative coupling of benzyl chlorides with aryl boronic acids in aqueous media
Wu, Xiao-Feng,Neumann, Helfried,Beller, Matthias
experimental part, p. 6146 - 6149 (2010/12/24)
A novel chemoselective protocol for the carbonylative Suzuki coupling of benzyl chlorides with aryl boronic acids at low pressure of carbon monoxide has been developed. Applying a commercially available palladium acetate/PCy 3 catalyst system in the presence of potassium phosphate as the base and water as the solvent the coupling reactions proceeded smoothly. To demonstrate the general applicability 12 different α-arylated acetophenones have been synthesized in moderate to good yields (41-78%) under mild conditions.
Reactions on a solid surface. A simple, economical and efficient Friedel-Crafts acylation reaction over zinc oxide (ZnO) as a new catalyst
Sarvari, Mona Hosseini,Sharghi, Hashem
, p. 6953 - 6956 (2007/10/03)
Zinc oxide (ZnO) brings about a rapid Friedel-Crafts acylation of a range of activated and unactivated aromatic compounds such as anisole and chlorobenzene with acid chlorides in solvent-free conditions at room temperature. The ZnO powder can be reused up to three times after simple washing with dichloromethane.
